Vaginal atrophy can occur in postmenopausal woman and estrogen deprived women who actually do not need any systemic hormone replacement therapy but just local therapy. Consequently, local, topical treatment is preferred in order to avoid the systemic side effects due to long-lasting oestrogen therapy. Local therapy for this purpose has been studied for a long period of time and the hormone has been administered as creams, gels, and silastic rings.
About every second postmenopausal women will experience urogenital discomfort associated with estrogen deficiency. Previous studies have shown that although many of these women use an oral hormone replacement therapy, urogenital symptoms persist.
A composition commonly used is Vagifem® marketed by Novo Nordisk A/S. Vagifem is developed to treat estrogen deficiency-deprived atrophic vaginitis. Vagifem is a small tablet containing 25 μg 17β-estradiol. For example, reference can be made to Maturitas 14 (1991), 23-31, where the women initially received 25 μg estradiol for 2 weeks and, thereafter, 25 μg estradiol once weekly or twice weekly. A usual treatment is one tablet of Vagifem containing 25 μg estradiol daily for the first 2 weeks of treatment and, thereafter, one tablet twice a week.
Conveniently, Vagifem is administered by placing a tablet at the top of a slim-line pencil-like disposable applicator. By introducing the applicator to the vagina, the Vagifem tablet will, due to the adhesive characteristics of Vagifem, stay in the vagina.
A pharmaceutical medicament for local, essentially non-systemic, treatment of vaginal dryness, in particular in the menopausal woman, characterized by a unit galenical formulation comprising a natural estrogen selected from the group consisting of 17β-estradiol and its salts and its derivatives in solution or in suspension in a lipophilic agent, with an estrogen content which corresponds to an equivalent unit dose of at most 15 μg, preferably less than 10 μg, of 17β-estradiol, a hydrophilic gel-forming bioadhesive agent, a gelling agent for the lipophilic agent, and a hydrodispersible agent, is described in U.S. Pat. No. 6,060,077. Hence, according to the U.S. Pat. No. 6,060,077 specification, 17β-estradiol and its salts and its derivatives are in solution or in suspension. Consequently, it cannot be a tablet.